Table 1.
IC50 (μM) | COX-2 in A549 cells* | COX-1(ovine)† | COX-2(human)† |
---|---|---|---|
9′-COOH | 6 ± 2 | >20‡ | >20‡ |
13′-COOH | 4 ± 2 | 5 ± 2 | 4 ± 2 |
γ-CEHC (3′-COOH) | 35–70§ | 300 ± 50 | 450 ± 50 |
α-CMBHC (5′-COOH) | n.d. | 160 ± 40 | 140 ± 40 |
Ibuprofen | 5 ± 2 | 8 ± 2 | 5 ± 1 |
Acetaminophen | 200 ± 50 | >250‡ | >250‡ |
The effect of purified 9′-COOH and 13′-COOH on COX activity was assayed in intact cells or using purified ovine COX-1 and human recombinant COX-2 (details described in Materials and Methods). Results were obtained based on two or three independent experiments and expressed as mean ± SD.
*The intact-cell assays were conducted in COX-2 preinduced A549 cells with 5 μM AA for 5 min.
†Assays were conducted with purified enzymes in the presence of 5 μM AA for 2 min.
‡9′-COOH and acetaminophen at 20 and 250 μM (the maximal concentrations tested), respectively, did not show any inhibitory effect on purified COX-1 or COX-2.
n.d., not determined.